Quercetin Loaded Monolaurate Sugar Esters-Based Niosomes: Sustained Release and Mutual Antioxidant—Hepatoprotective Interplay
Flavonoids possess different interesting biological properties, including antibacterial, antiviral, anti-inflammatory and antioxidant activities. However, unfortunately, these molecules present different bottlenecks, such as low aqueous solubility, photo and oxidative degradability, high first-pass...
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MDPI AG
2020-02-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/12/2/143 |
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| author | Enas Elmowafy Marwa O. El-Derany Francesca Biondo Mattia Tiboni Luca Casettari Mahmoud E. Soliman |
| author_facet | Enas Elmowafy Marwa O. El-Derany Francesca Biondo Mattia Tiboni Luca Casettari Mahmoud E. Soliman |
| author_sort | Enas Elmowafy |
| collection | DOAJ |
| description | Flavonoids possess different interesting biological properties, including antibacterial, antiviral, anti-inflammatory and antioxidant activities. However, unfortunately, these molecules present different bottlenecks, such as low aqueous solubility, photo and oxidative degradability, high first-pass effect, poor intestinal absorption and, hence, low systemic bioavailability. A variety of delivery systems have been developed to circumvent these drawbacks, and among them, in this work niosomes have been selected to encapsulate the hepatoprotective natural flavonoid quercetin. The aim of this study was to prepare nanosized quercetin-loaded niosomes, formulated with different monolaurate sugar esters (i.e., sorbitan C12; glucose C12; trehalose C12; sucrose C12) that act as non-ionic surfactants and with cholesterol as stabilizer (1:1 and 2:1 ratio). Niosomes were characterized under the physicochemical, thermal and morphological points of view. Moreover, after the analyses of the in vitro biocompatibility and the drug-release profile, the hepatoprotective activity of the selected niosomes was evaluated in vivo, using the carbon tetrachloride (CCl<sub>4</sub>)-induced hepatotoxicity in rats. Furthermore, the levels of glutathione and glutathione peroxidase (GSH and GPX) were measured. Based on results, the best formulation selected was glucose laurate/cholesterol at molar ratio of 1:1, presenting spherical shape and a particle size (PS) of 161 ± 4.6 nm, with a drug encapsulation efficiency (EE%) as high as 83.6 ± 3.7% and sustained quercetin release. These niosomes showed higher hepatoprotective effect compared to free quercetin in vivo, measuring serum biomarker enzymes (i.e., alanine and aspartate transaminases (ALT and AST)) and serum biochemical parameters (i.e., alkaline phosphatase (ALP) and total proteins), while following the histopathological investigation. This study confirms the ability of quercetin loaded niosomes to reverse CCl<sub>4</sub> intoxication and to carry out an antioxidant effect. |
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| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-13T09:10:32Z |
| publishDate | 2020-02-01 |
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| series | Pharmaceutics |
| spelling | doaj.art-e7a7dd0fd69043d3ac086bfe707ad32d2022-12-22T02:52:53ZengMDPI AGPharmaceutics1999-49232020-02-0112214310.3390/pharmaceutics12020143pharmaceutics12020143Quercetin Loaded Monolaurate Sugar Esters-Based Niosomes: Sustained Release and Mutual Antioxidant—Hepatoprotective InterplayEnas Elmowafy0Marwa O. El-Derany1Francesca Biondo2Mattia Tiboni3Luca Casettari4Mahmoud E. Soliman5Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Monazzamet Elwehda Elafrikeya Street, P.O.B. 11566 Abbaseyya, Cairo, EgyptDepartment of Biochemistry, Faculty of Pharmacy, Ain Shams University, Monazzamet Elwehda Elafrikeya Street, P.O.B. 11566 Abbaseyya, Cairo, EgyptDepartment of Biomolecular Sciences, School of Pharmacy, University of Urbino, Piazza Rinascimento, 6, 61029 Urbino (PU), ItalyDepartment of Biomolecular Sciences, School of Pharmacy, University of Urbino, Piazza Rinascimento, 6, 61029 Urbino (PU), ItalyDepartment of Biomolecular Sciences, School of Pharmacy, University of Urbino, Piazza Rinascimento, 6, 61029 Urbino (PU), ItalyDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Monazzamet Elwehda Elafrikeya Street, P.O.B. 11566 Abbaseyya, Cairo, EgyptFlavonoids possess different interesting biological properties, including antibacterial, antiviral, anti-inflammatory and antioxidant activities. However, unfortunately, these molecules present different bottlenecks, such as low aqueous solubility, photo and oxidative degradability, high first-pass effect, poor intestinal absorption and, hence, low systemic bioavailability. A variety of delivery systems have been developed to circumvent these drawbacks, and among them, in this work niosomes have been selected to encapsulate the hepatoprotective natural flavonoid quercetin. The aim of this study was to prepare nanosized quercetin-loaded niosomes, formulated with different monolaurate sugar esters (i.e., sorbitan C12; glucose C12; trehalose C12; sucrose C12) that act as non-ionic surfactants and with cholesterol as stabilizer (1:1 and 2:1 ratio). Niosomes were characterized under the physicochemical, thermal and morphological points of view. Moreover, after the analyses of the in vitro biocompatibility and the drug-release profile, the hepatoprotective activity of the selected niosomes was evaluated in vivo, using the carbon tetrachloride (CCl<sub>4</sub>)-induced hepatotoxicity in rats. Furthermore, the levels of glutathione and glutathione peroxidase (GSH and GPX) were measured. Based on results, the best formulation selected was glucose laurate/cholesterol at molar ratio of 1:1, presenting spherical shape and a particle size (PS) of 161 ± 4.6 nm, with a drug encapsulation efficiency (EE%) as high as 83.6 ± 3.7% and sustained quercetin release. These niosomes showed higher hepatoprotective effect compared to free quercetin in vivo, measuring serum biomarker enzymes (i.e., alanine and aspartate transaminases (ALT and AST)) and serum biochemical parameters (i.e., alkaline phosphatase (ALP) and total proteins), while following the histopathological investigation. This study confirms the ability of quercetin loaded niosomes to reverse CCl<sub>4</sub> intoxication and to carry out an antioxidant effect.https://www.mdpi.com/1999-4923/12/2/143glucose lauratesucrose lauratetrehalose lauratesorbitan lauratequercetinethanol injectionniosomesantioxidant effecthepatoprotection |
| spellingShingle | Enas Elmowafy Marwa O. El-Derany Francesca Biondo Mattia Tiboni Luca Casettari Mahmoud E. Soliman Quercetin Loaded Monolaurate Sugar Esters-Based Niosomes: Sustained Release and Mutual Antioxidant—Hepatoprotective Interplay Pharmaceutics glucose laurate sucrose laurate trehalose laurate sorbitan laurate quercetin ethanol injection niosomes antioxidant effect hepatoprotection |
| title | Quercetin Loaded Monolaurate Sugar Esters-Based Niosomes: Sustained Release and Mutual Antioxidant—Hepatoprotective Interplay |
| title_full | Quercetin Loaded Monolaurate Sugar Esters-Based Niosomes: Sustained Release and Mutual Antioxidant—Hepatoprotective Interplay |
| title_fullStr | Quercetin Loaded Monolaurate Sugar Esters-Based Niosomes: Sustained Release and Mutual Antioxidant—Hepatoprotective Interplay |
| title_full_unstemmed | Quercetin Loaded Monolaurate Sugar Esters-Based Niosomes: Sustained Release and Mutual Antioxidant—Hepatoprotective Interplay |
| title_short | Quercetin Loaded Monolaurate Sugar Esters-Based Niosomes: Sustained Release and Mutual Antioxidant—Hepatoprotective Interplay |
| title_sort | quercetin loaded monolaurate sugar esters based niosomes sustained release and mutual antioxidant hepatoprotective interplay |
| topic | glucose laurate sucrose laurate trehalose laurate sorbitan laurate quercetin ethanol injection niosomes antioxidant effect hepatoprotection |
| url | https://www.mdpi.com/1999-4923/12/2/143 |
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